CN112218863B - O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃糖苷酶抑制剂 - Google Patents

O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃糖苷酶抑制剂 Download PDF

Info

Publication number
CN112218863B
CN112218863B CN201980019170.5A CN201980019170A CN112218863B CN 112218863 B CN112218863 B CN 112218863B CN 201980019170 A CN201980019170 A CN 201980019170A CN 112218863 B CN112218863 B CN 112218863B
Authority
CN
China
Prior art keywords
methyl
acetamide
thiazol
fluoropyrimidin
compound
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CN201980019170.5A
Other languages
English (en)
Chinese (zh)
Other versions
CN112218863A (zh
Inventor
N.杰农
K.M.古基恩
J.维塞尔斯
L.张
R.吉亚纳塔西奥
E.Y.S.林
Z.辛
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Biogen MA Inc
Original Assignee
Biogen MA Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Biogen MA Inc filed Critical Biogen MA Inc
Priority to CN202410813893.5A priority Critical patent/CN118955490A/zh
Publication of CN112218863A publication Critical patent/CN112218863A/zh
Application granted granted Critical
Publication of CN112218863B publication Critical patent/CN112218863B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
CN201980019170.5A 2018-03-14 2019-03-13 O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃糖苷酶抑制剂 Active CN112218863B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202410813893.5A CN118955490A (zh) 2018-03-14 2019-03-13 O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃糖苷酶抑制剂

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201862642932P 2018-03-14 2018-03-14
US62/642,932 2018-03-14
US201862690536P 2018-06-27 2018-06-27
US62/690,536 2018-06-27
US201862699443P 2018-07-17 2018-07-17
US62/699,443 2018-07-17
PCT/US2019/021995 WO2019178191A1 (en) 2018-03-14 2019-03-13 O-glycoprotein-2-acetamido-2-deoxy-3-d-glycopyranosidase inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN202410813893.5A Division CN118955490A (zh) 2018-03-14 2019-03-13 O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃糖苷酶抑制剂

Publications (2)

Publication Number Publication Date
CN112218863A CN112218863A (zh) 2021-01-12
CN112218863B true CN112218863B (zh) 2024-07-12

Family

ID=65952097

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201980019170.5A Active CN112218863B (zh) 2018-03-14 2019-03-13 O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃糖苷酶抑制剂
CN202410813893.5A Pending CN118955490A (zh) 2018-03-14 2019-03-13 O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃糖苷酶抑制剂

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN202410813893.5A Pending CN118955490A (zh) 2018-03-14 2019-03-13 O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃糖苷酶抑制剂

Country Status (10)

Country Link
US (1) US20230117898A1 (https=)
EP (2) EP3765458B1 (https=)
JP (1) JP7453916B2 (https=)
CN (2) CN112218863B (https=)
AU (1) AU2019234759C1 (https=)
CA (1) CA3093315A1 (https=)
ES (1) ES2942211T3 (https=)
MA (1) MA52004A (https=)
MX (1) MX2020009530A (https=)
WO (1) WO2019178191A1 (https=)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018154133A1 (en) * 2017-02-27 2018-08-30 Janssen Pharmaceutica Nv [1,2,4]-triazolo [1,5-a]-pyrimidinyl derivatives substituted with piperidine, morpholine or piperazine as oga inhibitors
PE20211591A1 (es) * 2018-09-19 2021-08-18 Biogen Ma Inc Inhibidores de o-glicoproteina-2-acetamido-2-desoxi-3-d-glucopiranosidasa
WO2021094312A1 (en) 2019-11-11 2021-05-20 Janssen Pharmaceutica Nv Pyrrolidine and bicycloheteroaryl containing oga inhibitor compounds
WO2021110656A1 (en) 2019-12-02 2021-06-10 Janssen Pharmaceutica Nv Oga inhibitor compounds
WO2021123291A1 (en) 2019-12-18 2021-06-24 Janssen Pharmaceutica Nv Oga inhibitor compounds
AU2020409728A1 (en) 2019-12-18 2022-08-11 Janssen Pharmaceutica Nv OGA inhibitor compounds
CN114929337A (zh) 2019-12-18 2022-08-19 詹森药业有限公司 Oga抑制剂化合物
KR102533471B1 (ko) * 2020-11-23 2023-05-19 (주) 메디프론디비티 O-GlcNAcase 저해 활성을 갖는 화합물 및 이의 용도
CN114213315A (zh) * 2021-12-31 2022-03-22 上海陶术生物科技有限公司 含氮杂环类化合物及其中间体的合成方法
CN114560805B (zh) * 2022-01-20 2024-11-29 上海陶术生物科技有限公司 含氮杂环化合物及其中间体的合成方法
CN121405694A (zh) * 2024-07-26 2026-01-27 浙江同源康医药股份有限公司 Oga抑制剂及其应用

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105143222A (zh) * 2013-03-14 2015-12-09 默克专利有限公司 糖苷酶抑制剂
WO2017106254A1 (en) * 2015-12-18 2017-06-22 Merck Sharp & Dohme Corp. Glycosidase inhibitors and uses thereof
CN110300752A (zh) * 2016-12-16 2019-10-01 詹森药业有限公司 单环oga抑制剂化合物
CN110312716A (zh) * 2016-12-16 2019-10-08 詹森药业有限公司 双环oga抑制剂化合物
CN110325535A (zh) * 2017-02-27 2019-10-11 詹森药业有限公司 经哌啶、吗啉或哌嗪取代的作为oga抑制剂的[1,2,4]-三唑[1,5-a]-嘧啶基衍生物

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4938949A (en) 1988-09-12 1990-07-03 University Of New York Treatment of damaged bone marrow and dosage units therefor
EP2780014A4 (en) 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
EP2780013A4 (en) 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
WO2013078320A1 (en) 2011-11-21 2013-05-30 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
NZ628762A (en) 2012-02-10 2016-07-29 Constellation Pharmaceuticals Inc Modulators of methyl modifying enzymes, compositions and uses thereof
SI2953941T1 (sl) 2013-02-11 2017-08-31 Constellation Pharmaceuticals, Inc. Modulatorji metil-modificirajočih encimov, sestavki in uporabe le-teh
WO2014151142A1 (en) 2013-03-15 2014-09-25 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
EP3033334A1 (en) 2013-08-15 2016-06-22 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105143222A (zh) * 2013-03-14 2015-12-09 默克专利有限公司 糖苷酶抑制剂
WO2017106254A1 (en) * 2015-12-18 2017-06-22 Merck Sharp & Dohme Corp. Glycosidase inhibitors and uses thereof
CN110300752A (zh) * 2016-12-16 2019-10-01 詹森药业有限公司 单环oga抑制剂化合物
CN110312716A (zh) * 2016-12-16 2019-10-08 詹森药业有限公司 双环oga抑制剂化合物
CN110325535A (zh) * 2017-02-27 2019-10-11 詹森药业有限公司 经哌啶、吗啉或哌嗪取代的作为oga抑制剂的[1,2,4]-三唑[1,5-a]-嘧啶基衍生物

Also Published As

Publication number Publication date
WO2019178191A1 (en) 2019-09-19
AU2019234759A1 (en) 2020-09-17
EP3765458A1 (en) 2021-01-20
ES2942211T3 (es) 2023-05-30
US20230117898A1 (en) 2023-04-20
AU2019234759C1 (en) 2025-02-06
CN112218863A (zh) 2021-01-12
JP2021518340A (ja) 2021-08-02
MA52004A (fr) 2021-01-20
CN118955490A (zh) 2024-11-15
AU2019234759B2 (en) 2024-08-01
EP3765458B1 (en) 2023-01-11
MX2020009530A (es) 2021-01-15
WO2019178191A8 (en) 2019-12-26
EP4186899A1 (en) 2023-05-31
CA3093315A1 (en) 2019-09-19
JP7453916B2 (ja) 2024-03-21

Similar Documents

Publication Publication Date Title
CN112218863B (zh) O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃糖苷酶抑制剂
CN113072542B (zh) RORγt抑制剂及其制备方法和用途
JP7577655B2 (ja) 環状尿素
US10077269B2 (en) Imidazopyridazine compounds
CN113166137B (zh) O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃葡萄糖苷酶抑制剂
MX2014004254A (es) Derivados de carbamato / urea que contienen anillos de piperidina y piperazina como inhibidores del receptor h3.
EP3891146B1 (en) Morpholinyl, piperazinyl, oxazepanyl and diazepanyl derivatives useful as o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors
US11459324B2 (en) O-glycoprotein-2-acetamido-2-deoxy-3-D-glycopyranosidase inhibitors
JP7627269B2 (ja) ＲＯＲγｔ阻害剤、その製造方法及び使用
JP7663503B2 (ja) アゼチジニルｏ－糖タンパク質－２－アセトアミド－２－デオキシ－３－ｄ－グルコピラノシダーゼ阻害剤
KR20240165360A (ko) 에모파밀 결합 단백질 억제제 및 이의 용도
HK40046057A (en) O-glycoprotein-2-acetamido-2-deoxy-3-d-glycopyranosidase inhibitors
HK40046057B (en) O-glycoprotein-2-acetamido-2-deoxy-3-d-glycopyranosidase inhibitors

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant